FO-152
5'-O-(L-valyl)-5-氟尿苷盐酸Chemical Name: 5'-O-L-Valyl-5-fluorouridine hydrochloride; 5-Fluoro-1-beta-D-(5'-O-L-valyl)ribofuranosyluracil hydrochloride
CAS No. 80667-13-6, 84998-30-1 (free base, mono-p-toluenesulfonate salt)
项目整合开发状态: Phase II
项目研究机构: Daiichi Fine Chemicals (Originator)
合成路线:The acylation of 2',3'-O-isopropylidene-5-fluoro-uridine (II) with N-benzyloxycarbonylvaline (I) by means of 2,4,6-triisopropylbenzenesulfonyl chloride (TPS) in pyridine gives 5'-O(N-benzyloxycarbonylvalyl)-2',3'-O-isopropylidene-5-fluorouridine (III),which is treated with trifluoroacetic acid yielding 5'-O-(N-benzyloxycarbonylvalyl)-5-fluorouridine (IV).Finally,this compound is debenzylated by hydrogenation with H2 over Pd/C in isopropanol.
📌 参考资料/链接：
参考文献标题:Nucleoside derivs.,their preparation and their us
文献作者:Endo,T.; Sakai,K.; Chou,K.; Inamoto,Y.; Teshigawara,H.(Fuji Yakuhin Kogyo Co.,Ltd.)
参考来源:FR 2470774; US 4340728
📄 详细内容
合成路线:The acylation of 2',3'-O-isopropylidene-5-fluoro-uridine (II) with N-benzyloxycarbonylvaline (I) by means of 2,4,6-triisopropylbenzenesulfonyl chloride (TPS) in pyridine gives 5'-O(N-benzyloxycarbonylvalyl)-2',3'-O-isopropylidene-5-fluorouridine (III),which is treated with trifluoroacetic acid yielding 5'-O-(N-benzyloxycarbonylvalyl)-5-fluorouridine (IV).Finally,this compound is debenzylated by hydrogenation with H2 over Pd/C in isopropanol.
参考文献标题:FO-152
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1988,13(6),516
产品链接: CAS No. 80667-13-6››